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Dr. Derya Osmaniye Dr. Nurnehir Baltacı Bozkurt Berkant Kurban Gamze Benli Yardımcı Prof. Dr. Yusuf Ozkay Prof. Dr. Zafer Asım Kaplancıklı 《化学与生物多样性》2023,20(9):e202300944
In this study, 12 novel 2-((1-(4-(1H-imidazol-1-yl)phenyl)ethylidene)hydrazineylidene)-3-ethyl-4-(substitutephenyl)-2,3-dihydrothiazole derivatives were obtained. Among these compounds, 2-((1-(4-(1H-imidazol-1-yl)phenyl)ethylidene)hydrazineylidene)-4-([1,1′-biphenyl]-4-yl)-3-ethyl-2,3-dihydrothiazole ( 4h ) was chosen as the most active derivative in the series. According to the MTT results, compounds 4h and 4k showed activity with IC50=4.566±0.246 μM and IC50=4.537±0.463 μM, respectively. Unlike other derivatives, compound 4h carries a phenyl ring in the 4th position of the phenyl ring. This bulky group allowed the compound to settle in the enzyme active site. Dynamic studies show that the stability of the compound does not change over 40 ns. RMSD, RMSF and Rg parameters all remained within acceptable limits. The uninterrupted aromatic hydrogen bonding of the enzyme active site with the important amino acids Cys919, Glu885 and Asp1046 proves the inhibitory potential of compound 4h on the VEGFR-2 enzyme. It is thought that more active compounds will be reached with the derivatives to be synthesized starting from compound 4h . 相似文献
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A total of 201 thermophilic bacteria isolated from various thermal spring, mud and soil were tested for their antibacterial
activity. Among the mostly active isolates, Geobacillus toebii HBB-247 was further examined. Bacteriocin-like inhibitory substance (BLIS) produced by strain HBB-247 was found to be stable
up to 60°C, sensitive to proteolytic enzymes and effective against Enterococcus faecalis, Listeria sp., E. avium, Clostridium pasteurianum, Cellulomonas fimi and some thermophilic strains isolated and identified in this study. As a result of Tricine-SDS-PAGE molecular weight of
BLIS was estimated about 38 kDa. Production studies showed that G. toebii HBB-247 starts to produce antibacterial substance at early logarithmic phase of growth and maximum production was detected
at the end of the logarithmic phase. 相似文献